期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 45, 期 8, 页码 3439-3445出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.04.033
关键词
Leishmaniasis; Amastigote; Amino acid; Piperine; Promastigote
资金
- International Foundation for Science (IFS), Sweden [F/3971-1]
Based on reported antileishmanial activity of naturally occurring alkaloid piperine and amino acid esters, their conjugates were synthesized by the hydrolysis of piperine to piperic acid followed by reaction with amino acid methyl esters. These conjugates were further converted to compounds with free carboxyl group and those with reduced double bonds. The synthesized compounds were evaluated for activity against promastigote and amastigote forms of L. donovani in vitro. All the compounds showed better activity than either piperine or the amino acid methyl esters. Piperoyl-valine methyl ester was the most active compound showing an IC(50) of 0.075 mM against the amastigotes. Two active compounds were evaluated for in vivo activity in golden hamster model of leishmaniasis. (C) 2010 Elsevier Masson SAS. All rights reserved.
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